Espiro tablets p / o 50mg, No. 30
Expiration Date: 05/2027
Russian Pharmacy name:
Эспиро таблетки п/о 50мг, №30
Myocardial infarction: in addition to standard therapy, in order to reduce the risk of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (ejection fraction less than 40%) and clinical signs of heart failure after myocardial infarction.
Chronic heart failure: In addition to standard therapy to reduce cardiovascular mortality and morbidity in patients with NYHA functional class II chronic heart failure with reduced left ventricular ejection fraction (<35%).
Inside.
Food intake does not affect the absorption of Espiro.
Myocardial infarction
Treatment should begin with a dose of 25 mg once a day and increase cc to 50 mg once a day after 4 weeks, taking into account the potassium content in the blood serum (see Table 1). The recommended maintenance dose of Espiro is 50 mg once a day.
NYHA functional class II chronic heart failure
Treatment should be started with a dose of 25 mg once a day and increased to 50 mg once a day after 4 weeks, taking into account the serum potassium content
The maximum daily dose is 50 mg.
After a temporary discontinuation of Espiro due to an increase in serum potassium up to and more than 6.0 mmol / L, therapy with Espiro can be resumed at a dose of 25 mg every other day, when the serum potassium content is <5.0 mmol / l.
General recommendations
The serum potassium content should be determined before the appointment of the drug Espiro, during the first week and 1 month after the start of therapy or when changing the dose of the drug. In the future, it is also necessary to periodically monitor the serum potassium content.
Elderly patients
No initial dose adjustment is required in elderly patients. Due to the age-related decrease in renal function in elderly patients, the risk of developing hyperkalemia increases, especially in the presence of concomitant diseases that contribute to an increase in serum eplerenone concentrations, in particular, in case of mild to moderate hepatic dysfunction. It is recommended to periodically determine the content of potassium in the blood serum (see table 1).
Renal dysfunction
Adjustment of the initial dose in patients with mild renal dysfunction is not required. The degree of hyperkalemia increases with deteriorating renal function.
It is recommended to periodically determine the content of potassium in the blood serum (see table 1).
Eplerenone is not removed by hemodialysis. In patients with severe renal insufficiency (CC <30 ml / min), the use of the drug is contraindicated (see section 'Contraindications').
In patients with chronic heart failure of functional class II according to NYHA classification and moderate renal dysfunction (CC 30-60 ml / min), therapy should be started with a dose of 25 mg every other day, followed by dose adjustment depending on the serum potassium content ( see table 1). Experience of using the drug Espiro in patients with heart failure after myocardial infarction and CC <50 ml / min pet. Espiro should be used with caution in these patients.
In patients with CC <50 ml / min, the use of the drug Espiro at a dose of 25 mg once a day has not been studied.
Liver dysfunction
Adjustment of the initial dose in patients with mild to moderate hepatic dysfunction is not required. Given the increased concentration of eplerenone in these patients, it is recommended that serum potassium be monitored regularly, especially in elderly patients.
The use of the drug Espiro in patients with severely impaired liver function is contraindicated (see section 'Contraindications').
Concomitant therapy
With the simultaneous use of drugs that have a weak or moderately pronounced inhibitory effect on the CYP3A4 isoenzyme, for example, erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole, treatment with Espiro can be started with a dose of 25 mg once a day, while the dose of the latter should not exceed 25 mg once a day (see the section 'Interaction with other medicinal products').
1 tablet (50 mg) contains :
active substance : eplerenone - 50.00 mg.
excipients : lactose monohydrate - 77.34 mg; microcrystalline cellulose - 30.76 mg; hypromellose-15cP - 2.50 mg; sodium lauryl sulfate -1.70 mg; croscarmellose sodium - 6.00 mg; magnesium stearate - 1.70 mg.
Sheath : Opadray II 33G32578 (yellow) - 8.00 mg: hypromellose-6cP (E464) - 3.20 mg; titanium dioxide (E171) - 1.82 mg; lactose monohydrate - 1.68 mg; macrogol-3350 - 0.64 mg; triacetype - 0.48 mg; iron dye yellow oxide (E172) - 0.18 mg.
Hypersensitivity to eplerenone or other components of the drug;
clinically significant hyperkalemia;
the serum potassium content at the beginning of treatment is more than 5.0 mmol / l;
moderate or severe renal failure (creatinine clearance (CC) less than 30 ml / min in patients with chronic heart failure II functional class according to the NYHA classification);
severe liver failure (more than 9 points on the Child-Pugh scale);
concomitant use of potassium-sparing diuretics, potassium preparations or strong inhibitors of the CYP3A4 isoenzyme, for example, itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone;
plasma creatinine concentration> 2.0 mg / dL (or> 177 mmol / L) in men or> 1.8 mg / dL (or> 159 mmol / L) in women;
lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
there is no experience of using the drug in children under the age of 18, therefore, its appointment to patients of this age group is not recommended.
Carefully
Type 2 diabetes mellitus and microalbuminuria;
concomitant use of eplerenone and angiotensin-converting enzyme (LIF) inhibitors or angiotensin II receptor antagonists (APAII); preparations containing lithium; cyclosporine or tacrolimus; digoxin and warfarin in doses close to the maximum therapeutic, strong inducers of the CYP3A4 isoenzyme;
elderly age;
impaired renal function (CC less than 50 ml / min);
A triple combination of an AIF inhibitor and ARAP with eplerenone should not be used.
Trade name of the drug:
Espiro
International non-proprietary name:
eplerenone
Dosage form:
film-coated tablets
Composition:
1 tablet (25 mg) contains :
active substance : eplerenone - 25.00 mg.
excipients : lactose monohydrate - 38.67 mg; microcrystalline cellulose - 15.38 mg; gynromellose-15cP - 1.25 mg; sodium lauryl sulfate - 0.85 mg: croscarmellose sodium - 3.00 mg; magnesium stearate - 0.85 mg.
Sheath : Opadray II 33G32578 (yellow) - 4.00 mg: hypromellose-6cP (E464) - 1.60 mg; titanium dioxide (E171) - 0.91 mg; lactose monohydrate - 0.84 mg; macrogol-3350 - 0.32 mg; triacetyp - 0.24 mg; iron dye yellow oxide (E172) - 0.09 mg.
1 tablet (50 mg) contains :
active substance : eplerenone - 50.00 mg.
Excipients: lactose monohydrate - 77.34 mg; microcrystalline cellulose - 30.76 mg; hypromellose-15cP - 2.50 mg; sodium lauryl sulfate -1.70 mg; croscarmellose sodium - 6.00 mg; magnesium stearate - 1.70 mg.
Sheath : Opadray II 33G32578 (yellow) - 8.00 mg: hypromellose-6cP (E464) - 3.20 mg; titanium dioxide (E171) - 1.82 mg; lactose monohydrate - 1.68 mg; macrogol-3350 - 0.64 mg; triacetype - 0.48 mg; iron dye yellow oxide (E172) - 0.18 mg.
Description:
For tablets 25 mg : round, biconvex, yellow film-coated tablets. The color of the tablet at the break: from white to almost white.
For tablets 50 mg : round, biconvex, yellow film-coated tablets with a notch on one side. The color of the tablet at the break: from white to almost white.
Pharmacotherapeutic group:
diuretic potassium-sparing agent.
ATX code:
C03DA04
Pharmacological properties
Pharmacodynamics
Eplerenone has high selectivity for mineralocorticoid receptors in humans, in contrast to glucocorticoid, progesterone and androgen receptors and prevents the binding of mineralocorticoid to aldosterone, a key hormone of the renin-angiotensin-aldosterone system (RAAS), which is involved in the regulation of arterial pressure cardiovascular disease.
Eplerenone causes persistent increases in plasma renin and serum aldosterone. Subsequently, the secretion of renin is suppressed by aldosterone through a feedback mechanism. However, an increase in renin activity or circulating aldosterone concentration does not affect the effects of eplerenone.
Significant effect of eplerenone on heart rate (HR), duration of QRS intervals. PR or QT was not detected in healthy volunteers.
Pharmacokinetics
Absorption and distribution The
absolute bioavailability of eplerenone is 69% after oral administration of 100 mg eplerenone in tablet form. The maximum concentration (Cmax) in blood plasma is reached approximately 2 hours after ingestion. Cmax and area under the concentration-time pharmacokinetic curve (AUC) linearly depend on the dose in the range from 10 to 100 mg and non-linearly - at a dose over 100 mg. The equilibrium state is reached within 2 days.
Food intake does not affect absorption.
Eplerenone binds approximately 50% to blood plasma proteins, mainly to the alpha1-acid group of glycoproteins. The calculated volume of distribution in the equilibrium state is 50 (± 7) L. Eplerenone does not bind to red blood cells.
Metabolism and excretion
Eplerenone is metabolized primarily by the CYP3A4 isoenzyme. The active metabolites of eplerenone in blood plasma have not been identified. Less than 5% of the eplerenone dose is excreted unchanged through the kidneys and intestines. After a single oral administration of labeled eplerenone, about 32% of the dose was excreted through the intestines and about 67% through the kidneys. The half-life of eplerenone is approximately 3-5 hours, and the clearance from blood plasma is approximately 10 L / h.
Special patient groups
Age, sex and race: The pharmacokinetics of eplerenone at a dose of 100 mg once a day has been studied in elderly patients (over 65 years old) - men and women. The pharmacokinetic parameters of eplerenone in men and women did not differ significantly. In the steady state, in elderly patients, Cmax and AUC were, respectively, 22% and 45% higher than in young patients (18-45 years old).
Renal failure: The pharmacokinetics of eplerenone was studied in patients with renal insufficiency of varying severity and in patients undergoing hemodialysis. Compared with patients in the control group, patients with severe renal failure showed an increase in equilibrium AUC and Cmax by 38% and 24%, respectively, and in patients on hemodialysis, their decrease by 26% and 3%. No correlation was found between plasma clearance of eplerenone and creatinine clearance. Eplerenone is not removed by hemodialysis.
Hepatic impairment : The pharmacokinetics of eplerenone at a dose of 400 mg was compared in patients with moderate hepatic impairment (7-9 points on the Child-Pugh scale) and healthy volunteers. The equilibrium Cmax and AUC of eplerenone were increased by 3.6% and 42%, respectively.
In patients with severe hepatic impairment, eplerenone has not been studied, therefore its use in this group of patients is contraindicated.
Heart failure : The pharmacokinetics of eplerenone 50 mg was studied in patients with heart failure (NYHA functional class II-IV). Equilibrium AUC and Cmax in patients with heart failure were 38% and 30% higher, respectively, than in healthy volunteers matched for age, body weight and sex. The clearance of eplerenone in patients with heart failure is similar to that in healthy older adults.
Indications for use
Myocardial infarction: in addition to standard therapy, in order to reduce the risk of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (ejection fraction less than 40%) and clinical signs of heart failure after myocardial infarction.
Chronic heart failure: In addition to standard therapy to reduce cardiovascular mortality and morbidity in patients with NYHA functional class II chronic heart failure with reduced left ventricular ejection fraction (<35%).
Contraindications
Hypersensitivity to eplerenone or other components of the drug;
clinically significant hyperkalemia;
the serum potassium content at the beginning of treatment is more than 5.0 mmol / l;
moderate or severe renal failure (creatinine clearance (CC) less than 30 ml / min in patients with chronic heart failure II functional class according to the NYHA classification);
severe liver failure (more than 9 points on the Child-Pugh scale);
concomitant use of potassium-sparing diuretics, potassium preparations or strong inhibitors of the CYP3A4 isoenzyme, for example, itraconazole, ketoconazole, ritonavir, nelfinavir, clarithromycin, telithromycin and nefazodone;
plasma creatinine concentration> 2.0 mg / dL (or> 177 mmol / L) in men or> 1.8 mg / dL (or> 159 mmol / L) in women;
lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
there is no experience of using the drug in children under the age of 18, therefore, its appointment to patients of this age group is not recommended.
Carefully
Type 2 diabetes mellitus and microalbuminuria;
concomitant use of eplerenone and angiotensin-converting enzyme (LIF) inhibitors or angiotensin II receptor antagonists (APAII); preparations containing lithium; cyclosporine or tacrolimus; digoxin and warfarin in doses close to the maximum therapeutic, strong inducers of the CYP3A4 isoenzyme;
elderly age;
impaired renal function (CC less than 50 ml / min);
A triple combination of an AIF inhibitor and ARAP with eplerenone should not be used.
Application during pregnancy and during breastfeeding
There is no information on the use of the drug in pregnant women. The drug Espiro should be prescribed with caution and only in cases where the expected benefit to the mother significantly outweighs the possible risk to the fetus / child.
There is no known release of eplerenone after oral administration in breast milk. The possible adverse effects of eplerenone on breastfed infants are unknown, so it is advisable to either discontinue breastfeeding or discontinue the drug, depending on its importance to the mother.
Method of administration and dosage
Inside.
Food intake does not affect the absorption of Espiro.
Myocardial infarction
Treatment should begin with a dose of 25 mg once a day and increase cc to 50 mg once a day after 4 weeks, taking into account the potassium content in the blood serum (see Table 1). The recommended maintenance dose of Espiro is 50 mg once a day.
NYHA functional class II chronic heart failure
Treatment should be started with a dose of 25 mg once a day and increased to 50 mg once a day after 4 weeks, taking into account the serum potassium content
The maximum daily dose is 50 mg.
After a temporary discontinuation of Espiro due to an increase in serum potassium up to and more than 6.0 mmol / L, therapy with Espiro can be resumed at a dose of 25 mg every other day, when the serum potassium content is <5.0 mmol / l.
General recommendations
The serum potassium content should be determined before the appointment of the drug Espiro, during the first week and 1 month after the start of therapy or when changing the dose of the drug. In the future, it is also necessary to periodically monitor the serum potassium content.
Elderly patients
No initial dose adjustment is required in elderly patients. Due to the age-related decrease in renal function in elderly patients, the risk of developing hyperkalemia increases, especially in the presence of concomitant diseases that contribute to an increase in serum eplerenone concentrations, in particular, in case of mild to moderate hepatic dysfunction. It is recommended to periodically determine the content of potassium in the blood serum (see table 1).
Renal dysfunction
Adjustment of the initial dose in patients with mild renal dysfunction is not required. The degree of hyperkalemia increases with deteriorating renal function.
It is recommended to periodically determine the content of potassium in the blood serum (see table 1).
Eplerenone is not removed by hemodialysis. In patients with severe renal insufficiency (CC <30 ml / min), the use of the drug is contraindicated (see section 'Contraindications').
In patients with chronic heart failure of functional class II according to NYHA classification and moderate renal dysfunction (CC 30-60 ml / min), therapy should be started with a dose of 25 mg every other day, followed by dose adjustment depending on the serum potassium content ( see table 1). Experience of using the drug Espiro in patients with heart failure after myocardial infarction and CC <50 ml / min pet. Espiro should be used with caution in these patients.
In patients with CC <50 ml / min, the use of the drug Espiro at a dose of 25 mg once a day has not been studied.
Liver dysfunction
Adjustment of the initial dose in patients with mild to moderate hepatic dysfunction is not required. Given the increased concentration of eplerenone in these patients, it is recommended that serum potassium be monitored regularly, especially in elderly patients.
The use of the drug Espiro in patients with severely impaired liver function is contraindicated (see section 'Contraindications').
Concomitant therapy
With the simultaneous use of drugs that have a weak or moderately pronounced inhibitory effect on the CYP3A4 isoenzyme, for example, erythromycin, saquinavir, amiodarone, diltiazem, verapamil and fluconazole, treatment with Espiro can be started with a dose of 25 mg once a day, while the dose of the latter should not exceed 25 mg once a day (see the section 'Interaction with other medicinal products').
Side effect
The following undesirable effects are given in accordance with the following gradations of the frequency of their occurrence in accordance with the classification of the World Health Organization: very often ( > 10%); often ( > 1%, <10%); infrequently ( > 0.1%, <1%); rarely ( > 0.01%, <0.1%); very rare (<0.01%, including individual messages); the frequency is unknown (according to the available data, it is not possible to establish the frequency of occurrence).
Infectious diseases : infrequently - pyelonephritis, gynecomastia.
Disorders of the blood and lymphatic system : infrequently - eosinophilia.
Endocrine system disorders : infrequently - hypothyroidism.
Metabolic and nutritional disorders : often - hyperkalemia, hypercholesterolemia, hypertriglyceridemia, dehydration; infrequently - hyponatremia.
Mental disorders : infrequently - insomnia.
Nervous system disorders : often - dizziness, fainting; infrequently - headache, hypesthesia.
Heart disorders : often - myocardial infarction; infrequently - atrial fibrillation, left ventricular failure, tachycardia.
Vascular disorders : often - a marked decrease in blood pressure (BP); infrequently - orthostatic hypotension, thrombosis of the arteries of the lower extremities.
Respiratory, Thoracic, and Mediastinal Disorders: often - cough; infrequently - pharyngitis.
Disturbances from the gastrointestinal tract : often - diarrhea, nausea, constipation; infrequently - flatulence, vomiting.
Disorders from a hundred / young of the liver and biliary tract : infrequently - cholecystitis.
Violations of the skin and subcutaneous tissues : often - itchy skin; infrequently - increased sweating, skin rash; frequency unknown - angioedema.
Musculoskeletal and connective tissue disorders : often - cramps in the calf muscles of the legs, musculoskeletal pain; infrequently - back pain.
Disorders of the kidneys and urinary tract : often - impaired renal function.
General disorders and disorders at the injection site : infrequently - asthenia, malaise.
Laboratory and instrumental data : infrequently - an increase in the concentration of residual urea nitrogen, creatinine, a decrease in the expression of the epidermal growth factor receptor, an increase in the concentration of glucose in the blood serum.
Overdose
Cases of overdose of eplerenone in humans have not been described. The most likely manifestations of an overdose may be a marked decrease in blood pressure and hyperkalemia.
Treatment: with the development of a pronounced decrease in LD, supportive treatment should be prescribed. If hyperkalemia develops, standard therapy is indicated.
Eplerenone is not removed by hemodialysis. It was found that eplerenone actively binds to activated carbon.
Interaction with other medicinal products
‘армакодинамические взаимодействи¤
алийсберегающие диуретики и препараты кали¤: учитыва¤ повышенный риск развити¤ гиперкалиемии, эплеренон не следует назначать пациентам, получающим калийсберегающие диуретики и препараты кали¤. алийсберегающие диуретики могут усилить эффекты гипотензивных средств и других диуретиков.
ѕрепараты, содержащие литий: взаимодействие эплеренона с препаратами лити¤ не изучалось. ќднако, у пациентов, получавших препараты лити¤ в сочетании с диуретиками и ингибиторами ј»‘, описаны случаи повышени¤ концентрации и интоксикации литием. ?сли подобна¤ комбинаци¤ необходима, целесообразно контролировать содержание лити¤ в плазме крови.
?иклоспорин, такролимус: циклоспорин и такролимус могут вызвать нарушение функции почек и повысить риск развити¤ гиперкалиемии. —ледует избегать одновременного применени¤ эплеренона и циклоспорина или такролимуса. ?сли во врем¤ лечени¤ эплереноном потребуетс¤ назначение циклоспорина или такролимуса, рекомендуетс¤ регул¤рно контролировать содержание кали¤ в сыворотке крови и функцию почек.
Ќестероидные противовоспалительные препараты (Ќѕ¬ѕ): лечение III I¬ѕ может привести к острой почечной недостаточности за счет пр¤мого подавлени¤ клубочковой фильтрации, особенно у пациентов группы риска (пожилые пациенты и/или пациенты с дегидратацией). ѕри совместном применении этих средств до начала и во врем¤ лечени¤ необходимо обеспечивать адекватный водный режим и контролировать функцию почек.
“риметоприм: одновременное применение триметоприма с эплереноном повышает риск развити¤ гиперкалиемии. –екомендуетс¤ контролировать содержание кали¤ в сыворотке крови и функцию почек, особенно у пациентов с почечной недостаточностью и у пожилых пациентов.
»нгибиторы ј»‘ и антагонисты рецепторов ангиотензина II: при применении эплеренона с ингибиторами јѕ‘ или антагонистами рецепторов ангиотензина II следует регул¤рно контролировать содержание кали¤ сыворотки крови. ѕодобна¤ комбинаци¤ может привести к увеличению риска развити¤ гиперкалиемии, особенно у пациентов с нарушением функции почек, в т.ч. у пожилых пациентов.
Ќе следует примен¤ть тройную комбинацию ингибитора јѕ‘ и ј–јѕ с эплереноном.
јльфа1-адреноблокапюры (празозин, альфузозин): при одновременном применении альфа 1-адреноблокаторов с эплереноном может усилитьс¤ антигипертензивнос действие и/или увеличитьс¤ риск развити¤ ортостатической гипотензии, в св¤зи с чем, рекомендуетс¤ контролировать ј? при перемене положени¤ тела.
“рициклические антидепрессанты, нейролептики, амифостин, баклофеи: при одновременном применении этих средств с эплереноном может усилитьс¤ антигипертензивный эффект или увеличитьс¤ риск развити¤ ортостатической гипотензии.
vлюкокортикостероиды, тетракозактид: одновременное применение этих средств с эплереноном может привести к задержке натри¤ и жидкости.
‘армакокинетические взаимодействи¤
»сследовани¤ in vitro свидетельствуют о том, что эплеренон не ингибирует изоферменты CYP1A2, CYP2C19, CYP2C9, CYP2D6 и CYP3A4. Ёплеренон не ¤вл¤етс¤ субстратом или ингибитором гликопротеина –.
?игоксин: AUC дигоксина при одновременном применении с эплереноном увеличиваетс¤ на 16% (90% ?»: 4-30%). Ќеобходимо соблюдать осторожность, если дигоксин примен¤етс¤ в дозах, близких к максимальным терапевтическим.
¬арфарин: клинически значимого фармакокинетического взаимодействи¤ с варфарином не вы¤влено. Ќеобходимо соблюдать осторожность, если варфарин примен¤етс¤ в дозах, близких к максимальным терапевтическим.
—убстраты изофермента CYP3A4: в специальных исследовани¤х признаков фармакокинетического взаимодействи¤ эплеренона с субстратами изофермента CYP3A4, например, мидазоламом и цизапридом, вы¤влено не было.
»нгибиторы изофермента CYP3A4
—ильные ингибиторы изофермента CYP3A4: при применении эплеренона со средствами, ингибирующими изофермент CYP3A4, возможно значимое фармакокинетическое взаимодействие. —ильный ингибитор CYP3A4 (кетоконазол 200 мг два раза в сутки) вызывал увеличение AUC эплеренона па 441%. ќдновременное применение эплеренона с сильными ингибиторами изофермента CYP3A4, такими как кетоконазол, итракоиазол, ритонавир, нелфинавир, кларитромицин, телитромицин и нефазадон, противопоказано (см. раздел Ђѕротивопоказани¤ї),
—лабые и умеренные ингибиторы изофермента CYP3A4: одновременное применение с эритромицином, саквинавиром, амиодароном, дилтиаземом, верапамилом и флуконазолом сопровождалось значимым фармакокинетическим взаимодействием (степень увеличени¤ AUC варьировала от 98% до 187%). ѕри одновременном применении этих средств с эплереноном доза последнего не должна превышать 25 мг (см. раздел Ђ—пособ применени¤ и дозыї).
»ндукторы изофермента CYP3A4: одновременный прием препаратов, содержащих «веробой продыр¤вленный (сильный индуктор CYP3A4) с эплереноном вызывал снижение AIJC последнего на 30%. ѕри применении более сильных индукторов CYP3A4, таких как рифампицин, возможно более выраженное снижение AUC эплеренона.
”читыва¤ возможное снижение эффективности эплеренона, одновременное применение сильных индукторов CYP3A4 (рифампицина, карбамазепина, фенитоина, фенобарбитала, препаратов, содержащих «веробой продыр¤вленный) не рекомендуетс¤.
јнтациды: на основании фармакокинетического клинического исследовани¤ значительного взаимодействи¤ антацидов с эплереноном при их одновременном применении не предполагаетс¤.
ќсобые указани¤
vиперкалиеми¤
ѕри лечении препаратом Ёспиро может развитьс¤ гиперкалиеми¤, котора¤ обусловлена его механизмом действи¤. ¬ начале лечени¤ и при изменении дозы препарата у всех пациентов следует контролировать содержание кали¤ в сыворотке крови. ¬ дальнейшем периодический контроль содержани¤ кали¤ рекомендуетс¤ проводить пациентам с повышенным риском развити¤ гиперкалиемии, например, пожилым пациентам, пациентам с почечной недостаточностью и сахарным диабетом. ”читыва¤ повышенный риск развити¤ гиперкалиемии. назначение препаратов кали¤ после начала лечени¤ препаратом Ёспиро не рекомендуетс¤. —нижение дозы препарата Ёспиро приводит к снижению содержани¤ кали¤ в сыворотке крови. ¬ одном исследовании добавление гидрохлоротиазида к эплеренону преп¤тствовало увеличению содержани¤ кали¤ в сыворотке крови.
Ќарушение функции почек
” пациентов с нарушением функции почек, в том числе диабетической микроальбуминурией, рекомендуетс¤ регул¤рно контролировать содержание кали¤ в сыворотке крови. –иск развити¤ гиперкалиемии увеличиваетс¤ при снижении функции почек. ’от¤ число пациентов с сахарным диабетом 2 типа и микроальбуминурией в исследовани¤х было ограниченным, тем не менее, в этой небольшой выборке было отмечено увеличение частоты гиперкалиемии. ¬ св¤зи с этим у таких пациентов лечение следует проводить с осторожностью. Ёплеренон не удал¤етс¤ при гемодиализе. ѕрименение препарата Ёспиро противопоказано при т¤желой почечной недостаточности (см. раздел Ђѕротивопоказани¤ї).
Ќарушение функции печени
” пациентов с легким или умеренным нарушением функции печени (5-6 и 7-9 баллов по шкале „айлд-ѕью) увеличени¤ содержани¤ кали¤ в сыворотке крови более 5,5 ммоль/л вы¤влено не было. ” таких пациентов следует контролировать содержание электролитов. ” пациентов с т¤желым нарушением функции печени эплеренон не изучалс¤, поэтому его применение противопоказано (см. раздел Ђѕротивопоказани¤ї).
»ндукторы изофермента CYP3A4
ќдновременное применение препарата Ёспиро с сильными индукторами изофермента CYP3A4 не рекомендуетс¤ (см. раздел Ђ¬заимодействие с другими лекарственными препаратамиї).
?иклоспорин, такролимус, препараты, содержащие литий
¬о врем¤ лечени¤ препаратом Ёспиро следует избегать назначени¤ этих средств (см. раздел Ђ¬заимодействие с другими лекарственными препаратамиї).
Ћактоза
“аблетки содержат лактозу, поэтому их не следует назначать пациентам с редкими наследственными заболевани¤ми, такими как непереносимость лактозы, недостаточность лактазы и синдром мальабсорбции глюкозы-галактозы.
¬ли¤ние на способность управл¤ть транспортными средствами и механизмами
¬ли¤ние препарата Ёспиро на способность управл¤ть автотранспортом или пользоватьс¤ сложной техникой не изучалось. ќднако, учитыва¤ возможность препарата вызывать головокружение и обморочные состо¤ни¤, следует соблюдать осторожность при управлении автотранспортными средствами или пользовании сложной техникой на фоне приема препарата Ёспиро.
‘орма выпуска
Film-coated tablets, 25 mg and 50 mg.
10 tablets in a blister made of PVC film and aluminum foil.
3 or 9 blisters, together with instructions for use, are placed in a cardboard box.
Storage conditions
At a temperature not higher than 25 ? C.
Keep out of the reach of children.
Shelf life
3 years.
Do not use the drug after the expiration date.
Vacation conditions
Dispensed by prescription.